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A-192621
SKU
HY-120295-10 mg
Category Reference compound
Tags Apoptosis;Endothelin Receptor, Apoptosis;GPCR/G Protein, Endocrinology; Cardiovascular Disease
$290 – $2,500
Products Details
Product Description
– A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level[1][2][3].
Web ID
– HY-120295
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Metabolism-protein/nucleotide metabolism
Molecular Formula
– C33H38N2O6
References
– [1]Wu-Wong JR, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies. Clin Sci (Lond). 2002 Aug;103 Suppl 48:107S-111S.|[2]Sakai S, et al. Antagonists to endothelin receptor type B promote apoptosis in human pulmonary arterial smooth muscle cells. Life Sci. 2016 Aug 15;159:116-120.|[3]Wessale JL, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies. Clin Sci (Lond). 2002 Aug;103 Suppl 48:112S-117S.
CAS Number
– 195529-54-5
Molecular Weight
– 558.66
Compound Purity
– 99.85
SMILES
– O=C([C@H]1[C@H](C2=CC=C(OCCC)C=C2)N(CC(NC3=C(CC)C=CC=C3CC)=O)C[C@@H]1C4=CC=C(OCO5)C5=C4)O
Clinical Information
– No Development Reported
Research Area
– Endocrinology; Cardiovascular Disease
Solubility
– DMSO : ≥ 100 mg/mL
Target
– Apoptosis;Endothelin Receptor
Isoform
– ETA;ETB
Pathway
– Apoptosis;GPCR/G Protein
Product type
– Reference compound
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